Valemetostat NEW
| Price | $96 | $197 | $347 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: Valemetostat | CAS No.: 1809336-39-7 |
| Purity: 99.08% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱(chēng) | Valemetostat |
| 描述 | Valemetostat (DS-3201) is an EZH1/2 inhibitor that can be used to study relapsed/refractory peripheral T-cell lymphoma. |
| 體外活性 | METHODS: Valemetostat (DS-3201) was used to treat a group of malignant lymphoma cell lines derived from EZH1+ differentiated lymphocytes at low doses (0.1-100 nM), and the expression of H3K27me3 in sensitive lymphoma cells was observed. RESULTS valemetostat effectively inhibited H3K27me3 in sensitive lymphoma types, showing a targeted effect. [1] METHODS: The EZH inhibitor valemetostat (0.1-1000nM) was chemically screened and derivatized using half the maximal inhibitory concentration (IC50) of EZH1/2 and cellular H3K27me3. RESULTS valemetostat strongly and specifically inhibits EZH1 and EZH2 (IC50 < 10 nM). [2] METHODS: Human MCL cell lines Mino, JeKo-1, and REC-1 were treated with varying concentrations of valemetostat ranging from 3000 to 0.3 nmol/L or 3000 to 100 nmol/L, respectively. RESULTS Valemetostat at a concentration lower than 100 nmol/L significantly inhibited the growth of Mino and JeKo-1, while valemetostat at a concentration higher than 100 nmol/L inhibited the growth of REC-1. [3] |
| 體內(nèi)活性 | METHODS: In diffuse large B-cell lymphoma (DLBCL) cell xenograft model mice, Valemetostat (DS-3201) (25 mg/kg/50 mg/kg/100 mg/kg) was orally administered once a day to observe the tumor growth in the mice. RESULTS Valemetostat 100 mg/kg orally once daily was associated with nearly complete tumor regression without weight loss; lower doses (25 mg/kg) slowed tumor growth. [1] METHODS: Primary MCL cells were transplanted into 6-week-old SCID-Beige (SCIDbg) mice (CB17.Cg-Prkdc) by subcutaneous injection, and the mice were treated with valemetostat 200 mg/kg twice daily for three days. week. RESULTS valemetostat treatment significantly inhibited tumor growth, and all valemetostat-treated mice survived to the end of the study period. [3] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (92.21 mM) |
| 關(guān)鍵字 | Valemetostat | inhibit | Histone Methyltransferase | DS 3201 | Inhibitor | T-cell | DS3201 | lymphoma |
| 相關(guān)產(chǎn)品 | BIX-01294 trihydrochloride | Tazemetostat | Piribedil | XY1 | UNC 0631 | GSK126 | MAK683 | EZM 2302 | EPZ015666 | AMI-1 free acid | MS37452 | MRTX-1719 |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 血液病分子庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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